Taxol nanosuspension and preparation method thereof

A technology of nano-suspension and paclitaxel, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, and medical preparations containing active ingredients. The process is simple, the effect of enhancing safety and reducing energy consumption

Active Publication Date: 2010-09-29
南京百思福医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to solve the shortcomings of the existing dosage forms of paclitaxel, such as low drug loading, strong toxic and side effects, poor stability, complicated preparation process, and high price, to achieve a technol

Method used

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  • Taxol nanosuspension and preparation method thereof
  • Taxol nanosuspension and preparation method thereof
  • Taxol nanosuspension and preparation method thereof

Examples

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Example Embodiment

[0033] Example 1

[0034] Weigh 18825mg of poloxamer and PEG40025mg, add 50ml of tri-distilled water, magnetically stir to make it completely dissolved, weigh 50mg of paclitaxel raw material and dissolve in 2.5ml ethyl acetate and 2.5ml ethanol mixed solution, 10000rpm high shear milk Under the condition of uniformity, the oil phase is slowly injected into the water phase at a constant speed to precipitate the drug crystals, the initial suspension is rotary evaporated to remove the organic solvent, and the high pressure homogenization is carried out. The conditions are 300 bar circulation 6 times, 500 bar circulation 6 times, and 800 bar circulation 20 times. The milky white nano-suspension was obtained with a measured particle size of 256.1 nm and a zeta potential of -25.61 mv.

Example Embodiment

[0035] Example 2

[0036] Weigh poloxamer 18820mg and PEG40040mg, add 50ml of tri-distilled water, magnetically stir to dissolve them, weigh 30mg of paclitaxel raw material and dissolve in a mixed solution of 2ml ethyl acetate and 2ml ethanol, 10000rpm high shear milk uniform In this case, the oil phase is slowly injected into the water phase at a constant rate to precipitate the drug crystals, the initial suspension is rotary evaporated to remove the organic solvent, and the high pressure homogenization is performed under the conditions of 300 bar cycle 6 times, 500 bar cycle 6 times, 800 bar cycle 6 times, and 1500 bar cycle 20 times, the milky white nano-suspension was obtained, the measured particle size was 186.3 nm, and the zeta potential was -20.87 mv.

Example Embodiment

[0037] Example 3

[0038] Weigh poloxamer 18820mg, PEG40060mg, add 50ml of tri-distilled water, magnetically stir to completely dissolve, weigh 40mg of paclitaxel raw material and dissolve in 2ml ethyl acetate and 2ml ethanol mixed solution, 10000rpm high shear milk uniform In this case, the oil phase is slowly injected into the water phase at a constant speed to precipitate the drug crystals, the initial suspension is rotary evaporated to remove the organic solvent, and the high pressure homogenization is performed under the conditions of 300 bar circulation 6 times, 500 bar circulation 6 times, 800 bar circulation 6 times, and 1000 bar circulation. 20 times, the milky white nano-suspension was obtained, the particle size was 234.1nm, and the zeta potential was -25.21mv.

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Abstract

The invention relates to the field of medicinal preparations, in particular to a taxol nanosuspension and a preparation method thereof. The taxol nanosuspension is characterized in that: a surfactant consists of poloxamer 188 and polyethylene glycol in a weight ratio of 1:1-1:3. According to the invention, the defects of low medicament loading rate, strong toxic or side effect, low stability, complex preparation process, high cost and the like in the conventional taxol preparation are overcome, and the technical breakthrough in the field is achieved; and the taxol nanosuspension has the advantages of increasing medicament content, reducing administration toxicity and production cost and improving the adaptability and compliance of a patient so as to realize clinical use.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a paclitaxel intravenously administered nanosuspension injection, its preparation method and application. Background technique [0002] Paclitaxel (PTX) is a diterpenoid extracted from the bark of Taxus genus Taxus. It is a new type of microtubule stabilizer with unique anti-tumor activity. It is considered by the National Cancer Institute of the United States to be the most important progress in tumor chemotherapy in the past 15 to 20 years. At present, the United States has listed the drug as a first-line drug for various tumors. [0003] Although paclitaxel has good antitumor activity, its solubility in water is very small. According to literature reports, paclitaxel is soluble in organic solvents such as methanol, ethanol, and dimethyl sulfoxide, while its solubility in water is less than 30 μg / mL. The extremely low water solubility of paclitaxel brings great dif...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/337A61K47/34A61K47/36A61P35/00A61K47/10
Inventor 李学明程晓丹王永禄
Owner 南京百思福医药科技有限公司
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